Ulixertinib (BVD-523, VRT752271)
Molecular Weight(MW): 433.33
Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Cited by 16 Publications
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Immunoblotting studies depicting BTK, PLCγ2, ERK1/2, and p90RSK signaling in nontransduced, vector only, BTKWT, or BTKCys481Ser (BTKC481S) MYD88-mutated WM (BCWM.1) and ABC DLBCL (TMD8) cells following treatment with vehicle control, ibrutinib, or ERK1/2 inhibitors (ulixerinib, GDC-0994) alone or with ibrutinib for 2 hours. GAPDH was used as protein loading control.
Blood, 2018, 131(18):2047-2059. Ulixertinib (BVD-523, VRT752271) purchased from Selleck.
C) p-ERK levels after 0.1 or 2.5 µM ulixertinib (UT) treatment related to untreated (Ct) analyzed by flow cytometry at basal levels (unstimulated) or after stimulation with anti-IgM (stimulated). Bars represent the mean ± SEM of 6 samples analyzed in each group, 6 with mutations in genes of RAS-BRAFMAPK-ERK pathway (KITLG, PTPN11, BRAF, MAP2K1, MAP2K2, and MAPK1) and 6 U-IGHV CLL cases. Histograms showing anti-IgM stimulation of ERK (T202/Y204) phosphorylation and its inhibition by 100 nM and 2.5 µM ulixertinib (UT) in representative CLL cases (U-IGHV: CLL and case 15: BRAF mutation). Each patient is represented in a different color depending on the RAS-BRAF-MAPK-ERK mutational status and the mutation position related to BRAF.
Haematologica, 2018, doi:10.3324/haematol.2018.196931. Ulixertinib (BVD-523, VRT752271) purchased from Selleck.
Ulixertinib inhibited the proliferation of SUDHL-10 and Raji cells. (A) The activation of ERK1/2 was analyzed by Western blotting. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited ERK1/2 activation in a dose-dependent manner compared with control cells. Cell proliferation was measured by the CCK-8 assay. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited proliferation of SUDHL-10 (B) and Raji cells (C) in a time- and dose-dependent manner compared with control cells.
Int J Clin Exp Med, 2016, 9(6):10955-10962.. Ulixertinib (BVD-523, VRT752271) purchased from Selleck.
Purity & Quality Control
Choose Selective ERK Inhibitors
|Description||Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.|
In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. 
ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
|In vitro||DMSO||86 mg/mL (198.46 mM)|
|Ethanol||15 mg/mL (34.61 mM)|
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